Discovery of 6-[4-(6-nitroxyhexanoyl)piperazin-1-yl)]-9H-purine, as pharmacological post-conditioning agent
| Autor: | Anastasia Zoga, Efstathios K. Iliodromitis, Theano Fotopoulou, S.I. Bibli, Dimitrios Th. Kremastinos, Ioanna Andreadou, Maria Koufaki |
|---|---|
| Rok vydání: | 2012 |
| Předmět: |
Purine
Cardiotonic Agents Clinical Biochemistry Myocardial Infarction Pharmaceutical Science Post conditioning Purine analogue Endogeny 030204 cardiovascular system & hematology Pharmacology Biochemistry 03 medical and health sciences chemistry.chemical_compound 0302 clinical medicine Drug Discovery Animals Ischemic Postconditioning Molecular Biology 030304 developmental biology 0303 health sciences Nitrates Chemistry Myocardium Organic Chemistry Hemodynamics Heart Infarct size 3. Good health Purines Molecular Medicine Ischemic preconditioning Rabbits |
| Zdroj: | Bioorganic & Medicinal Chemistry. 20:5948-5956 |
| ISSN: | 0968-0896 |
| Popis: | Novel purine analogues bearing nitrate esters were designed and synthesized in an effort to develop compounds triggering endogenous cardioprotective mechanisms such as ischemic preconditioning (IPC) or postconditioning (PostC). The majority of the compounds reduced infarct size compared to the control group in anesthetized rabbits, whereas administration of the most active analogue 16 at a dose of 3.8 μmol/kg resulted on a significant reduction of infarct size, compared to PostC group (13.4 ± 1.9% vs 26.4 ± 2.3%). These findings introduce a novel class of promising pharmacological compounds that could be used as mimics or enhancers of PostC. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|
Full Text from ScienceDirect